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获得 4-甲氧基碳同位素标记 combretastatin A-4 磷酸酯和其他 Z- combretastatin 的有效合成策略。

An efficient synthetic strategy for obtaining 4-methoxy carbon isotope labeled combretastatin A-4 phosphate and other Z-combretastatins.

机构信息

Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, Tempe, Arizona 85287-1604, USA.

出版信息

J Nat Prod. 2010 Mar 26;73(3):399-403. doi: 10.1021/np9004486.

DOI:10.1021/np9004486

PMID:20028026

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2862752/

Abstract

Human cancer and other clinical trials under development employing combretastatin A-4 phosphate (1b, CA4P) should benefit from the availability of a [(11)C]-labeled derivative for positron emission tomography (PET). In order to obtain a suitable precursor for addition of a [(11)C]methyl group at the penultimate step, several new synthetic pathways to CA4P were evaluated. Geometrical isomerization (Z to E) proved to be a challenge, but it was overcome by development of a new CA4P synthesis suitable for 4-methoxy isotope labeling.

摘要

正在开发的人类癌症和其他临床试验采用 combretastatin A-4 磷酸盐 (1b, CA4P)，将受益于 [(11)C]-标记衍生物的可用性，用于正电子发射断层扫描 (PET)。为了获得合适的前体，以便在倒数第二步添加 [(11)C]甲基，评估了几种新的 CA4P 合成途径。几何异构化 (Z 到 E) 被证明是一个挑战，但通过开发适合 4-甲氧基同位素标记的新 CA4P 合成方法克服了这一挑战。